| ||
The screening group is integral part of Chemical Biology Program efforts in identifying the selective small molecule ligands for human proteins with these main benefits:
- Tight-binding ligands have the potential to stabilize and solubilize proteins, reduce aggregation and thereby enhance crystallization success rates of SGC targets.
- Selective small molecule tools can facilitate target validation of proteins for therapeutic intervention, by probing their roles in biochemical processes related to disease.
Activities of the group are focused on:
- Assembly and curation of protein family focused compound libraries, driven by literature review, selection and purchase of commercially available compounds, and also augmented by synthesis of new compounds by Med-chem. group.
- Hit identification by in-house medium throughput screening of the libraries is combined with collaborations with high-throughput screening groups.
- Where possible, de novo design to accelerate hit identification.
- Screening of the followup compounds to identify the most appropriate hits for further study and, where necessary, generation of SAR to optimize physicochemical properties.